ED90 of Norepinephrine and Phenylephrine Boluses for Treating Postspinal Anesthesia Hypotension Under Intensive Treatment in Preeclamptic Patients During Cesarean Section

The objective of this study is to investigate the ED90 of norepinephrine and phenylephrine boluses for treating postspinal anesthesia hypotension under intensive treatment in preeclamptic patients during cesarean section

Start Date01 Jul 2025

Sponsor / Collaborator

General Hospital of Ningxia Medical University

NCT06158009 / Not yet recruitingNot ApplicableIIT

ED90 of Norepinephrine and Phenylephrine Boluses for Treating Postspinal Anesthesia Hypotension Under Intensive Treatment During Cesarean Section

The objective of this study is to investigate the ED90 of norepinephrine and phenylephrine boluses for treating postspinal anesthesia hypotension under intensive treatment during cesarean section

Start Date01 Apr 2025

Sponsor / Collaborator

General Hospital of Ningxia Medical University

100 Clinical Results associated with α1B-AR x α1A-AR

100 Translational Medicine associated with α1B-AR x α1A-AR

0 Patents (Medical) associated with α1B-AR x α1A-AR

309

Literatures (Medical) associated with α1B-AR x α1A-AR

07 Feb 2024·ACS Chemical Neuroscience

Identification of a Novel Subtype-Selective α_1B-Adrenoceptor Antagonist

Article

Author: Deluigi, Mattia ; Vaid, Tasneem M ; Whitehead, Alice ; Bathgate, Ross A D ; Gooley, Paul R ; Scott, Daniel J ; Zhang, Yifan ; Hubbard, Roderick E ; Abdul-Ridha, Alaa ; Plückthun, Andreas ; Betrie, Ashenafi Haileyesus ; Chalmers, David K ; Davis, Ben ; Simmonite, Heather ; de Zhang, Lazarus A ; Harris, Richard

α_1A-, α_1B-, and α_1D-adrenoceptors (α₁-ARs) are members of the adrenoceptor G protein-coupled receptor family that are activated by adrenaline (epinephrine) and noradrenaline. α₁-ARs are clinically targeted using antagonists that have minimal subtype selectivity, such as prazosin and tamsulosin, to treat hypertension and benign prostatic hyperplasia, respectively. Abundant expression of α₁-ARs in the heart and central nervous system (CNS) makes these receptors potential targets for the treatment of cardiovascular and CNS disorders, such as heart failure, epilepsy, and Alzheimer's disease. Our understanding of the precise physiological roles of α₁-ARs, however, and their involvement in disease has been hindered by the lack of sufficiently subtype-selective tool compounds, especially for α_1B-AR. Here, we report the discovery of 4-[(2-hydroxyethyl)amino]-6-methyl-2H-chromen-2-one (Cpd1), as an α_1B-AR antagonist that has 10-15-fold selectivity over α_1A-AR and α_1D-AR. Through computational and site-directed mutagenesis studies, we have identified the binding site of Cpd1 in α_1B-AR and propose the molecular basis of α_1B-AR selectivity, where the nonconserved V197^45.52 residue plays a major role, with contributions from L314^6.55 within the α_1B-AR pocket. By exploring the structure-activity relationships of Cpd1 at α_1B-AR, we have also identified 3-[(cyclohexylamino)methyl]-6-methylquinolin-2(1H)-one (Cpd24), which has a stronger binding affinity than Cpd1, albeit with reduced selectivity for α_1B-AR. Cpd1 and Cpd24 represent potential leads for α_1B-AR-selective drug discovery and novel tool molecules to further study the physiology of α₁-ARs.

29 Dec 2023·Journal of Biomolecular Structure and Dynamics

Integrated LC-MS/MS and network pharmacology approach for predictingactive ingredients and pharmacological mechanisms of Tribulus terrestris L. against cardiac diseases

Article

Author: Nayak, Usha Yogendra ; Vinay, Chigateri M. ; B Joshi, Manjunath ; Bhat, Chandrakanth ; Rai, Padmalatha S. ; Paul, Bobby ; Kamath, Archana ; Mehta, Chetan Hasmukh

Tribulus terrestris L. (Gokshura) is a medicinal herb used for treating cardiac diseases and several other diseases. However, the active ingredients and the possible mechanism of action for treating cardiac diseases remain unclear. Hence, the study was designed to identify the active ingredients and to explore the potential mechanism of action of Tribulus terrestris L. for treating cardiac diseases by an integrated approach of metabolomics and network pharmacology. We performed HPLC-QTOF-MS/MS analysis to identify putative compounds and network pharmacology approach for predictive key targets and pathways. Using molecular docking and molecular dynamics simulation, we identified the active ingredients in Tribulus terrestris L. that can act as putative lead compounds to treat cardiac diseases. A total of 55 putative compounds were identified using methanolic extract of Tribulus terrestris L. using HPLC-QTOF-MS/MS analysis. Network pharmacology analysis predicted 32 human protein targets from 25 secondary metabolites, which have shown direct interaction with cardiac diseases. Based on the degrees of interaction, the hub targets such as TACR1, F2, F2R, ADRA1B, CHRM5, ADRA1A, ADRA1D, HTR2B, and AVPR1A were identified. In silico molecular docking and simulation resulted in the identification of active ingredients such as Kaempferol 3-rutinoside 7-glucuronide, Keioside, rutin, moupinamide, aurantiamide, quercetin-3-o-α-rhamnoside, tribuloside, and 3'',6''- Di-O-p-coumaroyltrifolin against hub protein targets. Hence, these compounds could be potential lead compounds for treating cardiac diseases. A further assessment of its efficacy can be made based on in vivo and in vitro studies for better understanding and strong assertion.Communicated by Ramaswamy H. Sarma.

11 Dec 2023·Journal of Complementary and Integrative Medicine

Alterations in expression of α1-adrenergic receptors possibly are involved in prevention of age-associated apoptosis in rat hippocampus by treadmill exercise

Article

Author: Chodari, Leila ; Mehranfard, Nasrin ; Ghasemi, Maedeh

AbstractObjectivesExercise is assumed to attenuate age-related neuronal apoptosis, but the detailed mechanism(s) is not fully understood. α1-Adrenergic receptors (ARs) can either trigger or suppress apoptosis, therefore, here we determined the impact of treadmill exercise on the expression of the apoptosis regulatory proteins as well as α1-AR subtypes α1A- and α1B-ARs, in order to elucidate a possible association between apoptosis and the hippocampal expression of α1-ARs in aged male rats.MethodsTwenty-one male Wistar rats were divided into 3 groups (n=7): young control, aged sedentary, and aged + exercise. Western blot for α1A- and α1B-ARs as well as pro-(Bax and p53) and anti-apoptotic (Bcl2) proteins was conducted. An 8-week regular moderate-intensity treadmill exercise intervention was carried out in exercise group.ResultsIn aged rats, α1A-AR expression in the hippocampus was significantly increased, and exercise markedly prevented this event. While α1B-AR expression was no altered with aging, a marked reduction in α1B-AR level was detected in exercise group when compared to aged group. Furthermore, pro-apoptotic protein levels of Bax and p53 were upregulated and anti-apoptotic protein Bcl2 was downregulated in the aging hippocampus, but could be reversed by treadmill exercise. In the present research, exercise-induced reduction in α1A- and α1B-ARs was associated with an obvious downregulation of Bax/Bcl2 ratio in aged rats, suggesting that exercise may inhibit apoptosis through regulating α1-ARs, particularly α1A-AR.ConclusionsOur study suggests that manipulations attenuating α1-AR activity, including nonselective α1-adrenergic antagonists, may protect against hippocampal neurodegeneration in aging brains.

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